Assay Detail
Binding
CHEMBL2394892
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PLK1 (unknown origin) using biotin-AGAGTVPESIHSFIGDGLV as substrate by TR-FRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase PLK1 (CHEMBL3024) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.98 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2392549 | — | — | 1 | 9.00 |
| CHEMBL2392548 | — | — | 1 | 9.00 |
| CHEMBL2392556 | — | — | 1 | 9.00 |
| CHEMBL2392545 | TAK-960 | 1.0 | 1 | 8.70 |
| CHEMBL2392554 | — | — | 1 | 8.70 |
| CHEMBL2392544 | — | — | 1 | 8.52 |
| CHEMBL2392553 | — | — | 1 | 8.40 |
| CHEMBL2392558 | — | — | 1 | 8.30 |
| CHEMBL2392552 | — | — | 1 | 7.92 |
| CHEMBL2392550 | — | — | 1 | 7.82 |
| CHEMBL2392547 | — | — | 1 | 7.58 |
| CHEMBL2392557 | — | — | 1 | 7.16 |
| CHEMBL2392546 | — | — | 1 | 7.09 |
| CHEMBL2392555 | — | — | 1 | 7.00 |
| CHEMBL2392543 | — | — | 1 | 6.77 |
| CHEMBL2392551 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2392549 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2392548 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2392556 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2392545 | TAK-960 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2392554 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2392544 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2392553 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2392558 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2392552 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2392550 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2392547 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2392557 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2392546 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2392555 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2392543 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2392551 | — | IC50 | = | 190.0 | nM | 6.72 |